[Rhinitis, vasomotor (treatment)]—Budesonide is used in the treatment of vasomotor rhinitis in patients who are unresponsive to conventional therapy. Antihistamines are generally considered the primary therapy for this disorder. {07}8Acceptance not established
Use of nasal budesonide in children younger than 4 years of age for the treatment of seasonal and perennial rhinitis has not been established.{07}7

Fluticasone—91%, to albumin; not significantly bound to transcortin. {78}5Biotransformation:

Beclomethasone—Hepatic to free beclomethasone and other inactive metabolites. {78}4{78}3{78}2{78}1{78}0{67}{83}{85} The portion of the dose that is swallowed and absorbed from the gastrointestinal tract undergoes extensive first-pass metabolism to inactive compounds {56}{63}. Initially hydrolyzed to beclomethasone-17-propionate by fecal esterases {25}{83}{85}.

Flunisolide—Rapid; hepatic to a less active 6-beta-hydroxy metabolite and to glucuronide and sulfate conjugates {20}. The portion of the dose that is swallowed and absorbed from the gastrointestinal tract undergoes extensive first-pass metabolism to inactive compounds. {56}{63}

Patients intolerant of benzalkonium chloride, disodium edetate, oleic acid or phenylethanol may be intolerant of some nasal corticosteroid preparations, since they may contain these substances as preservatives.

Budesonide—No evidence of carcinogenic effect was found in mice and rats given oral doses of up to 200 mcg/kg/day for 91 weeks. An increase in incidence of gliomas and hepatocellular tumors were observed in a 104-week study in male rats given doses of 50 mcg/kg/day orally. No such changes were seen in male rats at doses of 10 and 25 mcg/kg/day or at any dose in female rats. {16}{70}

Flunisolide—In long-term studies, flunisolide given orally caused an increase in the incidence of benign pulmonary adenomas in mice but not in rats. Also, as reported for other corticosteroids, flunisolide caused an increased incidence of mammary adenocarcinoma in female rats receiving the highest oral doses {20}.

Fluticasone—Tumorigenic potential was found in mice given oral doses of up to 1000 mcg/kg (20 times the maximum recommended daily (MRD) intranasal dose in adults and 10 times the MRD in children) for 78 weeks and in rats given inhalation doses up to 57 mcg/kg (2 times MRD intranasal dose in adults and equal to the MRD intranasal dose in children), for 104 weeks. {24}

Mometasone—No evidence of carcinogenicity was found in rats when given an inhalation dose of 67 mcg per kg body weight (mcg/kg) (approximately 3 times the MRD intranasal dose in adult humans on a mcg/m 2 basis). No evidence of an increase in tumors was found in mice given an inhalation dose of 160 mcg/kg (approximately 4 times the MRD intranasal dose in adult humans on a mcg/m 2 basis). {73}

Triamcinolone—No evidence of carcinogenicity was demonstrated in a 2-year study on male and female rats administered oral doses of 1 mcg per kg of body weight (mcg/kg) a day and male and female mice administered oral doses of 3 mcg/kg a day. {68}{69}{97}Mutagenicity

Budesonide—No mutagenicity or clastogenic properties was found in any tests. {16}{70}

Fluticasone—No gene mutation induction was found in prokaryotic or eukaryotic cells in vitro . {24}

Triamcinolone—Studies on mutagenicity have not been done. {68}{69}{97}Pregnancy/Reproduction
Fertility—Beclomethasone: Female dogs administered beclomethasone orally showed impaired fertility (inhibition of the estrous cycle). However, this effect was not observed following administration of the medication via inhalation. {02}{25}{66}{67}{75}{76}{83}{85}

Dexamethasone: Dexamethasone may increase or decrease spermatozoa count or motility in some patients. {86}

Fluticasone—No evidence of impairment of fertility was observed in studies of rats given subcutaneous doses of up to 50 mcg/kg (2 times the MRD intranasal dose in adult humans on a mcg/m 2 basis). {24}

Triamcinolone: Male and female rats administered triamcinolone acetonide orally at doses of up to 15 mcg/kg per day (maternally toxic doses are 2.5 to 15 mcg/kg per day) exhibited no evidence of impaired fertility.

Pregnancy—
Corticosteroids cross the placenta. Adequate and well-controlled studies in humans have not been done with beclomethasone {25}, budesonide, dexamethasone {86}, flunisolide {20}{21}{27}{63}fluticasone, mometasone {23}or triamcinolone nasal formulations. Use during pregnancy should be considered only if the benefit to the mother outweighs the potential risk to the fetus {75}, especially during the first trimester {70}{77}.

Studies in animals have shown that corticosteroids are embryotoxic, fetotoxic, and/or teratogenic. {02}{25}{66}{67}{75} However, teratogenic effects have not been confirmed in humans receiving systemic corticosteroids.

Infants born to mothers who have received substantial doses of corticosteroids during pregnancy should be carefully observed for signs of hypoadrenalism (anorexia, hypotension, weakness and weight loss). {35}{75}{86}

Beclomethasone

In one study of orally inhaled beclomethasone in humans, beclomethasone did not cause teratogenic or other adverse effects {63}.

Studies in mice and rabbits have shown that beclomethasone administered subcutaneously at 10 times the MRD adult human dose causes increased fetal resorptions and birth defects, including cleft palate, agnathia, microstomia, absence of tongue, delayed ossification, and partial agenesis of the thymus. {02}{63}{66}{67}{75}{83}{85} No teratogenic effects were observed in rats given an inhalation dose of 10 times the MRD adult human dose or an oral dose of 1000 times the MRD adult human dose. {75}{83}{85}

Studies on rabbits given a subcutaneous dose of 4 mcg/kg (less than the MRD in adult humans on a mcg/m 2 basis), revealed decrease in fetal weight and cleft palate. No teratogenic effects were reported at oral doses of up to 300 mcg/kg (25 times the MRD intranasal dose in adult humans on a mcg/m 2 basis). Fluticasone crossed the placenta following oral administration of 1000 mcg/kg given to rats and 300 mcg/kg given to rabbits (approximately 4 and 25 times the MRD intranasal dose in adult humans on a mcg/m 2 basis).

A few female rats administered oral doses of 8 mcg/kg per day exhibited dystocia and prolonged delivery and at oral doses of 5 mcg/kg per day exhibited an increase in fetal resorptions, stillbirths, decrease in pup body weight and survival. {68}{69}

. Studies in rats and rabbits administered systemic doses of 20 to 80 mcg/kg per day have shown teratogenic effects, including a low incidence of cleft palate and/or internal hydrocephaly and axial skeletal defects. Studies in non-human primates administered systemic doses of 500 mcg/kg per day have shown teratogenic effects, including CNS and cranial malformations {68}{69}{77}. Administration of triamcinolone nasal aerosol to pregnant rats and rabbits resulted in embryotoxic and fetotoxic effects that were comparable to those produced by administration by other routes. {69}

Distribution of significant quantities of corticosteroids into breast milk may suppress growth, interfere with endogenous corticosteroid production, or cause other adverse effects in the nursing infant {63}.

Dexamethasone—It is distributed into breast milk. {63}{86} Nursing while receiving pharmacologic doses of dexamethasone is not recommended. {63}{86}

Mometasone—Plasma concentrations are not measurable in breast milk following the administration of the MRD intranasal adult human dose; thus fetal or breast milk exposure is expected to be negligible and toxicity low. Use of mometasone while breast-feeding should be considered if the benefit to the mother outweighs the risk to the infant. {23}Pediatrics{54}
Significant suppression of growth has not been well documented {97}{102} with the use of usual doses of nasal beclomethasone and flunisolide {36}{40}{52}{63}. If significant systemic absorption of nasal corticosteroids occurs in pediatric patients, adrenal suppression and growth suppression may result {63}. Prolonged or high-dose therapy with these medications during pregnancy, especially dexamethasone, requires careful attention to dosage and close monitoring of growth and development of the infant. {02}{12}{16}{20}{21}{23}{24}{25}{66}{67}{68}{69}{70}{73}{75}{76}{83}{85}

Geriatrics

Appropriate studies with nasal corticosteroids have not been performed in the geriatric population. {63} However, geriatrics-specific problems that would limit the usefulness of this medication in the elderly are not expected. {24}{63}{76}Drug interactions and/or related problems
The following drug interactions and/or related problems have been selected on the basis of their potential clinical significance (possible mechanism in parentheses where appropriate)—not necessarily inclusive (» = major clinical significance):

Ephedrine or
Phenobarbital or
Rifampin (induction of hepatic microsomal enzyme activity, by ephedrine, phenobarbital and rifampin, may result in increased metabolism, decreased serum concentration, decreased elimination half-life of dexamethasone and may warrant an increase in dexamethasone dosage {86}.)

Laboratory value alterations
The following have been selected on the basis of their potential clinical significance (possible effect in parentheses where appropriate)—not necessarily inclusive (» = major clinical significance):

Glucose concentration, blood and urine (may be increased if significant absorption occurs because of intrinsic hyperglycemic activity of glucocorticoids; most likely with dexamethasone)

Hematologic status (should be monitored during long-term therapy)

Medical considerations/Contraindications
The medical considerations/contraindications included have been selected on the basis of their potential clinical significance (reasons given in parentheses where appropriate)— not necessarily inclusive (» = major clinical significance).

Risk-benefit should be considered when the following medical problems exist
Amebiasis, latent or active (dexamethasone or other corticosteroids may activate latent amebiasis {86})

Note: The risk of systemic effects is minimal with usual doses of nasal beclomethasone and flunisolide. Side effects from usual doses of beclomethasone are generally limited to local effects {52}{55}.
Systemic effects including hypothalamic-pituitary-adrenal (HPA) axis suppression may occur with usual doses of nasal dexamethasone {86} greater-than-recommended doses of beclomethasone, budesonide flunisolide, fluticasone or triamcinolone {20}{21}{23}{24}{56}{75}. (Doses of 440 mcg of triamcinolone acetonide administered daily for 42 days did not measurably affect adrenal response to a 6-hour cosyntropin test. {97}) If the patient is particularly sensitive or has recently used systemic corticosteroids prior to using nasal corticosteroids, the patient may also be predisposed to hypercorticism (blurred vision, bone fractures, excess facial hair growth in females, fullness or rounding of face, neck, and trunk, hypertension, increased thirst and urination, impotence in males, lack of menstrual periods, muscle wasting or weakness). {24}{25}{41}{70}{75}{83}{85}

The following side/adverse effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:Those indicating need for medical attentionIncidence more frequentFor beclomethasoneHeadache—incidence 34% {02}{66}{67}{76}

For beclomethasone and flunisolide{61}Irritation of throat—possibly due to vehicle in nasal spraysneezing attacks—may be more common in children using beclomethasone aerosol or flunisolide spray {37}{38}{40}{52}{59}{60}{75}{83}{85}

Overdose
For more information on the management of overdose or unintentional ingestion, contact a Poison Control Center (see Poison Control Center Listing ).Treatment of overdose
For acute overdose—Adverse effects due to acute overdose are unlikely with the small quantities of corticosteroid contained in each canister. {20}{21}{23}{25}{68}{69}{73}{75}{77}{78}{86}

Pregnancy—Risk-benefit must be considered, since systemic corticosteroids cross the placenta and have demonstrated embryotoxicity, fetotoxicity, and teratogenicity in animals; infants born to mothers who received substantial doses of corticosteroids during pregnancy should be observed for hypoadrenalism {35}

Breast-feeding—Risk-benefit must be considered, since systemic corticosteroids are distributed into breast milk and have demonstrated embryotoxicity, fetotoxicity, and teratogenicity in animals; infants breast-fed by mothers who received substantial doses of corticosteroids while breast-feeding should be observed for hypoadrenalism {35}

Use in children—Significant effect on growth by beclomethasone or flunisolide has not been documented; importance of monitoring growth and development with prolonged or high-dose therapy

General Dosing Information
In patients with blocked nasal passages, a topical decongestant may be used just prior to use of the nasal corticosteroid. {02}{12}{23}{66}{67}{68}{69}{75} However, because prolonged use of topical nasal decongestants may cause congestive rebound, they should preferably be used for a maximum of 3 to 5 days. An oral decongestant is recommended for chronic nasal congestion.

The dosage of other corticosteroids being administered concurrently by other routes of administration, including oral inhalation, should be taken into account when determining the usual adult prescribing limits of nasal corticosteroids. {90}

Note: If orally inhaled beclomethasone is used concurrently, the combined total daily dose should not exceed 1 mg. {84}

Usual pediatric dose
Anti-inflammatory (steroidal), nasal
Children up to 6 years of age: Safety and efficacy have not been established. {05}{25}{28}{66}{76}{84}

Children 6 years of age and older: See Usual adult and adolescent dose.{25}{84}Usual pediatric prescribing limits
Nasal, 400 mcg (0.4 mg) (8 metered sprays) per day. {84} If orally inhaled beclomethasone is used concurrently, the combined total daily dose should not exceed 500 mcg (0.5 mg). {84}Strength(s) usually available
U.S.—

Additional Dosing Information
Regular use is required to obtain full therapeutic benefit. Treatment should not be continued beyond 3 weeks in the absence of significant symptomatic improvement. {12}{70}{79}

Note: [Children 4 to 6 years of age]1 have benefited from 100 mcg (1 metered inhalation) to 200 mcg (2 metered inhalations) in each nostril daily, up to 400 mcg (4 metered inhalations total) daily, followed by a dosage adjusted to the lowest effective dose as determined by the child's response.{103}

Usual adult prescribing limits
Nasal, 800 mcg (0.8 mg) per day.Usual pediatric dose
Anti-inflammatory (steroidal), nasal
Children up to 6 years of age: Safety and efficacy have not been established. {12}{79}

Note: [Children 4 to 6 years of age]1 have benefited from 100 mcg (1 metered inhalation) to 200 mcg (2 metered inhalations) in each nostril daily, up to 400 mcg (4 metered inhalations total) daily, followed by a dosage adjusted to the lowest effective dose as determined by the child's response.{103}

Note: [Children 4 to 6 years of age]1 have benefited from 100 mcg (1 metered inhalation) to 200 mcg (2 metered inhalations) in each nostril daily, up to 400 mcg (4 metered inhalations total) daily, followed by a dosage adjusted to the lowest effective dose as determined by the child's response.{103}

Note: Some patients may be maintained on 100 mcg (0.1 mg) (1 metered spray) of dexamethasone phosphate in each nostril two times a day. Therapy should be discontinued as soon as possible {86}. If symptoms recur, therapy may be reinstituted.

Usual adult prescribing limits
Nasal, 1.2 mg (12 metered sprays) of dexamethasone phosphate per day {86}.Usual pediatric dose
Anti-inflammatory (steroidal), nasal
Children up to 6 years of age: Use is not recommended {86}.

Children 6 to 12 years of age: Nasal, 100 or 200 mcg (0.1 to 0.2 mg) (1 or 2 metered sprays) of dexamethasone phosphate in each nostril two times a day (total daily dose, 400 to 800 [0.4 to 0.8 mg] of dexamethasone phosphate {86}.

Children up to 6 years of age:
Safety and efficacy have not been established. {20}{21}{71}{72}

Children 6 to 14 years of age:
Initial—Nasal, 25 mcg (0.025 mg) (1 metered spray) in each nostril three times a day {80}; or 50 mcg (0.05 mg) (2 metered sprays) in each nostril two times a day; (total daily dose, 150 or 200 mcg [0.15 or 0.2 mg]). {20}{21}{71}{72}

Maintenance—Nasal, as little as 25 mcg (0.025 mg) (1 metered spray) in each nostril once a day has been effective (total daily dose, 50 mcg [0.05 mg]). {72}{80}

Note: In Canada, the dose may be increased to 100 mcg (0.1 mg) (2 metered sprays) in each nostril every twelve hours (total daily dose, 400 mcg [0.4 mg]), if no response at the usual and adolescent dose. {64}

Note: In Canada, the literature also includes that for each 55 mcg (0.55 mg) metered spray (dose reaching nasal mucosa), 100 mcg (0.1 mg) of triamcinolone acetonide is released from the actuator {77}.

Usual adult prescribing limits
Nasal, 440 mcg (0.44 mg) (8 metered sprays) per day. {68}{77}Usual pediatric dose
Anti-inflammatory (steroidal), nasal
Children up to 6 years of age (In Canada, children up to 12 years of age): Safety and efficacy have not been established. {68}{77}

Usual adult prescribing limits
Nasal, 220 mcg (0.22 mg) (4 metered sprays) per day. {69}Usual pediatric dose
Anti-inflammatory (steroidal), nasal
Children up to 6 years of age (In Canada, children up to 4 years of age): Use is not recommended {69}{78}.

Children 6 to 11 years of age (In Canada, children 4 to 11 years of age): Nasal, 55 mcg (0.055 mg) (1 metered spray) in each nostril once a day {69}{78}

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